14 results about "Benzodiazepine Compounds" patented technology

The present invention discloses benzodiazepine compounds and use in interferon activator protein agonists thereof, involving a compound of formula I, a racemate or optical isomer thereof, a pharmaceutically acceptable salt and solvate thereof, and use in the preparation of antiviral and anti-tumor drugs related to interferon activator protein (STING) thereof.

A benzodiazepine compound having a structure represented by formula (I) and functioning as a ROCK II kinase inhibitor, as well as the use of the compound in Rho kinase inhibitor drugs and a method for preparing the same. JPEG2026513014000117.jpg6297

The present invention relates to the technical field of the synthesis of benzodiazepine compounds, and specifically discloses a magnetic nano-bifunctional acid catalyst, a preparation method thereof, and a catalytic application. In the present invention, Fe3O4@SiO2 core-shell nanoparticles modified with a chlorosilane coupling agent are selected as the carrier, and an aminophosphonic acid compound is used as the grafting substance. Through the dehydrochlorination reaction between the Cl in the silane coupling agent and the NH2 in the aminophosphonic acid compound, the grafting of the aminophosphonic acid compound on the surface of the magnetic nanoparticles is realized. Then, with the aminophosphonic acid compound as the loading medium, the metal atom in the Lewis acid is coordinated with the N in the amino group and the O in the phosphoric acid group of the aminophosphonic acid compound respectively, forming a stable polycyclic structure, and the purpose of stably loading the transition metal Lewis acid and phosphonic acid on the surface of the magnetic nanoparticles is achieved. It has broad application prospects in the field of synthesizing 1,5-benzodiazepine compounds containing a spiro ring structure.

The invention provides a salt represented by the structure of Formula (I): wherein Q is an ammonium cation; and a process comprising the use of said salts for the preparation of benzodiazepine compounds, in particular bis (fluoroalkyl) derivatives thereof.

The application belongs to the technical field of DNA coded compound library, and particularly relates to a synthesis method of On-DNA benzodiazepine compounds, which comprises the following steps: taking On-DNA aldehyde compounds, diamine compounds and diketone compounds as substrates, and cyclizing to obtain On-DNA benzodiazepine compounds under mild and biocompatible reaction conditions, wherein the synthesis method is small in DNA damage, good in substrate universality, high in yield, low in cost, convenient in operation, suitable for the synthesis of On-DNA benzodiazepine compounds, rich in chemical reaction types of DEL library, and conducive to the drug development of benzodiazepine compounds.

Provided are a new type of benzodiazepine compound, a preparation method thereof, and a use thereof. The short-acting benzodiazepine derivative has the characteristics of rapid onset, short action time, strong depth, fast metabolism, and fast awakening. In the anesthesia experiments on mice and rats, the short-acting benzodiazepine derivative has an onset time comparable to that of remazepam, but the action time and awakening time are significantly shortened, and the action depth of some compounds is significantly enhanced, and has the characteristics of faster onset, shorter action time, greater action strength, faster metabolism, and faster awakening. In the long-term infusion anesthesia experiment on rats, compared with remazepam, the short-acting benzodiazepine derivative has significantly shortened awakening time and recovery time, and has the characteristics of faster awakening and faster recovery.

The present disclosure relates to benzodiazepine compounds and pharmaceutically acceptable salts thereof to their use in medicine; to pharmaceutical compositions containing them; to processes for their preparation; and to intermediates used in such processes. The benzodiazepine compounds may be useful in the treatment, prevention, suppression and amelioration of RSV infections.

The application discloses a novel compound shown in formula (I), a preparation method and application thereof, and belongs to the field of medicinal chemistry. The benzodiazepine compound has the characteristics of rapid effect, short action time, strong depth, fast metabolism and fast recovery. In the anesthesia experiment on mice and rats, the effect time of the compound is equivalent to that of remazepam, but the action time and recovery time are significantly shortened, the action depth of part of the compounds is obviously strengthened, the compound has the characteristics of faster effect, shorter action time, greater action strength, faster metabolism and faster recovery, and has good heart safety. In the long-term infusion anesthesia experiment on rats, compared with remazepam, the recovery time and recovery time of the short-acting benzodiazepine derivative of the application are significantly shortened, and the compound has the characteristics of faster recovery and faster recovery.

The invention discloses a benzodinitrogen compound, a pharmaceutical composition and application of the benzodinitrogen compound. Specifically provided are a compound represented by formula I, and a stereoisomer, a deuterated compound or a pharmaceutically acceptable salt thereof. The compound provided by the invention has one or more advantages and effects as follows: (1) the compound provided by the invention has a relatively good vein sedation and anesthesia effect; (2) the compound provided by the invention is small in drug accumulation effect and good in tolerance; and (3) the compound disclosed by the invention has an anesthetic effect of more quickly reviving.

The present disclosure relates to benzodiazepine compounds and pharmaceutically acceptable salts thereof, their uses in medicine, pharmaceutical compositions containing them, processes for their preparation, and intermediates used in such processes. The benzodiazepine compounds can be useful in the treatment, prevention, inhibition, and amelioration of RSV infection.

A benzodiazepine compound represented by formula I, or a salt thereof has an intravenous sedative anesthesia effect. The recovery quality of the compound is significantly improved compared with remimazolam in rat and mouse caudal venous anesthesia models. During anesthetization, the compound has a rapid onset, a short duration, a quick recovery and a good tolerance, can be used for anesthesia induction, anesthesia maintenance and day surgery anesthesia.

A salt of a neuroceutical and of an acid, wherein the neuroceutical is a substituted benzodiazepine, a substituted benzothiazepine, a substituted pyridopyrimidines or a substituted amino-cyclohexaneacetic acid; and the acid is benzoic acid, nicotinic acid, pantothenic acid and tannic acid. The molar ratio of the neuroceutical and the acid in the salt ranges from about 6:1 to about 1:5. Also disclosed herein are compositions comprising the neuroceutical salt and therapeutic uses thereof for treating a central nervous system (CNS) disorder or a metabolic disorder associated with the CNS disorder.

Provided is a novel pharmaceutical agent for glioma.　This glioma therapeutic agent is characterized by comprising, as an active ingredient, a synaptic activator of an inhibitory neuron. This synaptic activator is, for instance, a GABA receptor agonist, and specifically, a benzodiazepine compound such as diazepam.